膜结合型和可溶型阿片受体中二硫键的证据。

Evidence for disulfide bonds in membrane-bound and solubilized opioid receptors.

作者信息

Kamikubo K, Murase H, Murayama M, Matsuda M, Miura K

机构信息

Third Department of Internal Medicine, Gifu University School of Medicine, Japan.

出版信息

J Neurochem. 1988 Feb;50(2):503-9. doi: 10.1111/j.1471-4159.1988.tb02940.x.

DOI:10.1111/j.1471-4159.1988.tb02940.x

PMID:2826698

Abstract

The effects of pretreatment with dithiothreitol (DTT) on opioid binding activities of membrane-bound and digitonin-solubilized opioid receptors from bovine adrenal medulla were studied. Pretreatment of membranes with DTT or mercaptoethanol inhibited [3H]diprenorphine binding by reducing the number of binding sites. The inhibitory action of DTT was time and dose dependent. The binding of [3H]D-Ala2-D-Leu5-enkephalin was also inhibited by DTT pretreatment. Pretreatment of digitonin-solubilized binding sites with DTT also reduced the number of [3H]diprenorphine binding sites. The action of DTT was diminished by preincubating the DTT solution with H2O2. [3H]Diprenorphine protected the opioid binding sites from the inhibitory action of DTT. The present results provide evidence that disulfide bonds are implicated in opioid binding activity of the opioid receptor system.

摘要

研究了用二硫苏糖醇（DTT）预处理对来自牛肾上腺髓质的膜结合型和洋地黄皂苷增溶型阿片受体阿片结合活性的影响。用DTT或巯基乙醇预处理膜，通过减少结合位点的数量来抑制[³H]二丙诺啡结合。DTT的抑制作用具有时间和剂量依赖性。DTT预处理也抑制了[³H]D-Ala²-D-Leu⁵-脑啡肽的结合。用DTT预处理洋地黄皂苷增溶的结合位点也减少了[³H]二丙诺啡结合位点的数量。通过将DTT溶液与过氧化氢预孵育，DTT的作用减弱。[³H]二丙诺啡保护阿片结合位点免受DTT的抑制作用。目前的结果提供了证据，表明二硫键与阿片受体系统的阿片结合活性有关。